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Design,synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents
Authors:Evgeniy A Gusakov  Iuliia A Topchu  Aleksandra M Mazitova  Igor V Dorogan  Emil R Bulatov  Ilya G Serebriiskii  Zinaida I Abramova  Inna O Tupaeva  Oleg P Demidov  Duong Ngoc Toan  Tran Dai Lam  Duong Nghia Bang  Yanis A Boumber  Yurii A Sayapin  Vladimir I Minkin
Abstract:Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been synthesized and tested for their anti-proliferative activity against several human cancer cell lines. Two compounds (3d and mixture B of 3i–k) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds 3d and mixture B of 3i–k also demonstrated induction of apoptotic cell death of ovarian cancer (OVCAR-3, OVCAR-8) and colon cancer (HCT 116) cell lines and affected ERK signaling. In summary, 2-quinolyl-1,3-tropolones are promising compounds for development of effective anticancer agents.

Tropolones are promising organic compounds that can have important biologic effects.
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